- Tricyclic dihydroimidazopyrimidinone derivative, and preparation method, pharmaceutical composition and application thereof
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The invention provides a compound as shown in a general formula (I), cis-trans isomers, enantiomers, diastereoisomers, racemes, solvates, hydrates or pharmaceutically acceptable salts or prodrugs of the compound, a preparation method of the compound, a pharmaceutical composition containing the compound and an application of the compound as aLp-PLA2 inhibitor, wherein R1, R2, Rx, Ra, Q, U, X, Y, m, n and A are defined in the specification.
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Paragraph 0353-0356
(2021/05/12)
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- Preparation method of chiral N-tert-butyloxycarborylmorpholine-3-carboxylic acid
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The invention provides a preparation method of chiral N-tert-butyloxycarborylmorpholine-3-carboxylic acid, which comprises the following steps: (1) carrying out an amino protection reaction on chiralserinamide and an amino protective agent to obtain a com
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Paragraph 0105; 0113-0114; 0133; 0141-0142; 0146; 0154-0155
(2020/08/25)
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- Synthesis of 3-oxadiazolyl/triazolyl morpholines: Novel scaffolds for drug discovery
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Synthesis of isomeric 3-oxadiazolyl/triazolyl morpholines was performed based on a common intermediate on the gram scale. The target compounds were designed as novel scaffolds for the medicinal chemistry. The key reaction was an electrochemical CH-oxidati
- Tereshchenko, Alexander D.,Myronchuk, Julia S.,Leitchenko, Lena D.,Knysh, Irina V.,Tokmakova, Ganna O.,Litsis, Olena O.,Tolmachev, Andrey,Liubchak, Konstantin,Mykhailiuk, Pavel
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p. 750 - 757
(2017/01/16)
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- NOVEL PYRAZOLO PYRIMIDINE DERIVATIVES AND THEIR USE AS MALT1 INHIBITORS
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The present invention describes new pyrazolo-pyrimidine derivatives of formula (I) or a pharmaceutically acceptable salt thereof; (I) wherein, R1 is halogen, cyano, or C1-C3alkyl optionally substituted by halogen; R2 is C1-C6alkyl optionally substituted one or more times by C1-C6alkyl, C2-C6alkenyl, hydroxyl, N,N-di-C1-C6alkyl amino, N-mono-C1-C6alkyl amino, O-Rg, Rg, phenyl, or by C1-C6alkoxy wherein said alkoxy again may optionally be substituted by C1-C6alkoxy, N,N-di-C1-C6alkyl amino, Rg or phenyl; C3-C6cycloalkyl optionally substituted by C1-C6alkyl, N,N-di-C1-C6alkyl amino or C1-C6alkoxy-C1-C6alkyl, and/or two of said optional substituents together with the atoms to which they are bound may form an annulated or spirocyclic 4 - 6 membered saturated heterocyclic ring comprising 1 - 2 O atoms; phenyl optionally substituted by C1-C6alkoxy; a 5 - 6 membered heteroaryl ring having 1 to 3 heteroatoms selected from N and O said ring being optionally substituted by C1-C6alkyl which may be optionally substituted by amino or hydroxy; Rg; or N,N-di-C1-C6alkyl amino carbonyl; and R is phenyl independently substituted two or more times by Ra, 2-pyridyl independently substituted one or more times by Rb, 3-pyridyl independently substituted one or more times by Rc, or 4-pyridyl independently substituted one or more times by Rd; which are generally interacting with MALT1 proteolytic and/or autoproteolytic activity, and in particular which may inhibit said activity. The present invention further describes the synthesis of said new pyrazolo-pyrimidine derivatives, their use as a medicament, especially by interacting with MALT1 proteolytic and/or autoproteolytic activity.
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Page/Page column 53; 54
(2015/12/31)
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- COMBINATIONS OF HEPATITIS C VIRUS INHIBITORS
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The present disclosure is generally directed to antiviral compounds, and more specifically directed to combinations of compounds which can inhibit the function of the NS5A protein encoded by Hepatitis C virus (HCV), compositions comprising such combinations, and methods for inhibiting the function of the NS5A protein.
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Page/Page column 595
(2015/02/02)
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- ANTI-INFECTIVE COMPOUNDS
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The present invention relates to small molecule compounds having the general formula (I): wherein A is a moiety selected from the group consisting of formulae (A) to (K) and their use in the treatment of bacterial infections, in particular Tuberculosis.
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Page/Page column 54
(2016/06/28)
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- PYRAZOLO [1, 5 -A] PYRIMIDINES AS ANTIVIRAL AGENTS
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The invention provides compounds of Formula I or Formula II: (I), (II) or a pharmaceutically acceptable salt or ester, thereof, as described herein. The compounds and compositions thereof are useful for treating Pneumovirinae virus infections. The compounds, compositions, and methods provided are particularly useful for the treatment of Human respiratory syncytial virus infections.
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Page/Page column 161
(2012/01/14)
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- NEW BRADYKININ B1 ANTAGONISTS
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The invention relates to compounds of formula (I), wherein R1 to R5 and X1 to X4, n and m have the meaning as cited in the description and the claims. Said compounds are useful as Bradykinin B1 antagonists. The
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Page/Page column 47
(2008/12/08)
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- Synthesis of chiral C/N-functionalized morpholine alcohols: Study of their catalytic ability as ligand in asymmetric diethylzinc addition to aldehyde
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A broad variety of chiral C/N-functionalized morpholine alcohols sharing a common structural motif in the 3-(hydroxymethyl)morpholine 6 were prepared from enantiomerically pure serine for the purpose of studying their catalytic ligand properties. The asym
- Dave, Rajesh,Sasaki, N. Andre
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p. 388 - 401
(2007/10/03)
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- POLYHETEROCYCLIC COMPOUNDS AND THEIR USE AS METABOTROPIC GLUTAMATE RECEPTOR ANTAGONISTS
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The present invention relates to new compounds of formula (I), wherein P, Q, X1, X2, X3, X4, X5, X6, R1, R2, R3, m, n, and p are as defined as in formula (I), or salts, or hydrates thereof, processes for their preparation and new intermediates used in the preparation thereof, pharmaceutical compositions containing said compounds and to the use of said compounds in therapy.
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Page/Page column 41-42
(2010/02/13)
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- Inhibitors of protein isoprenyl transferases
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Compounds having the formula or a pharmaceutically acceptable salt thereof wherein R1 is (a) hydrogen, (b) loweralkyl, (c) alkenyl, (d) alkoxy, (e) thioalkoxy, (f) halo, (g) haloalkyl, (h) aryl-L2—, and (i) heterocyclic-L2—; R2 is selected from(a) (b) —C(O)NH—CH(R14)—C(O)OR15, (d) —C(O)NH—CH(R14)—C(O)NHSO2R16,(e) —C(O)NH—CH(R14)-tetrazolyl, (f) —C(O)NH-heterocyclic, and(g) —C(O)NH—CH(R14)—C(O)NR17R18; R3 is substituted or unsubstituted heterocyclic or aryl, substituted or unsubstituted cycloalkyl or cycloalkenyl, ?and —P(W)RR3RR3′; R4 is hydrogen, lower alkyl, haloalkyl, halogen, aryl, arylakyl, heterocyclic, or (heterocyclic)alkyl; L1 is absent or is selected from (a) —L4—N(R5)—L5—, (b) —L4—O—L5—, (c) —L4—S(O)n—L5—(d) —L4—L6—C(W)—N(R5)—L5—, (e) —L4—L6—S(O)m—N(R5)—L5—, (f) —L4—N(R5)—C(W)—L7—L5—, (g) —L4—N(R5)—S(O)p—L7—L5—, (h) optionally substituted alkylene, (i) optionally substituted alkenylene, (j) optionally substituted alkynylene (k) a covalent bond, (l) and (m) are inhibitors of protein isoprenyl transferases. Also disclosed are protein isoprenyl transferase inhibiting compositions and a method of inhibiting protein isoprenyl transferases.
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